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Nine pyridyloxypyridyl indole carboxamides were synthesized and displayed high affinities for 5-HT 2C receptors and high selectivity over 5-HT 2A and 5-HT 2B . Among them, 6-methyl- N -[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]1 H -indole-3-carboxamide ( 8 ) exhibits the highest 5-HT 2C binding affinity ( K  i = 1.3 nM) and high selectivity over 5-HT 2A (∼1000 times) and 5-HT 2B (∼140 times). [ 11 C] 8 was synthesized by palladium-catalyzed coupling reaction between pinacolboranate 16 and [ 11 C]CH 3 I with an average radiochemical yield of 27 ± 4% ( n = 8, decay-corrected from end of [ 11 C]CH 3 I synthesis). MicroPET imaging studies in rhesus monkeys showed regional uptake of [ 11 C] 8 in the choroid plexus, whereas the bindings in all other brain regions were low. The specific binding in the choroid plexus was confirmed by administration of a blocking dose of 0.1 mg/kg of the 5-HT 2C antagonist SB-242084.

Synthesis and Evaluation of Pyridyloxypyridyl Indole Carboxamides as Potential PET Imaging Agents for 5-HT2C Receptors

Synthesis and Evaluation of Pyridyloxypyridyl Indole Carboxamides as Potential PET Imaging Agents for 5-HT_2C Receptors